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Pramipexole dihydrochloride hydrate
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Pramipexole dihydrochloride hydrate
品牌： Absin
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对比
咨询分子式：
C10H17N3S.2HCl.H2O
分子量：
302.26
产品介绍
产品介绍
产品信息
抗原名称
D2S Receptor,D2L Receptor,D3 receptor,D4 receptor
商品描述
Pramipexole is a partial/full D2S, D2L, D3, D4, receptor agonist with a Ki of 3.9, 2.2, 0.5, 5.1 nM. It also possesses low/insignificant affinity (500-10,000 nM) for the 5-HT1A, 5-HT1B, 5-HT1D, and α2-adrenergic receptors. It has negligible affinity (>10,000 nM) for the D1, D5, 5-HT2, α1-adrenergic, β-adrenergic, H1, and mACh receptors. It is a non-ergoline dopamine agonist indicated for treating early-stage Parkinson’s disease (PD) and restless legs syndrome (RLS).
分子量
302.26
纯度
>98%
可溶性
DMSO ：39 mg/mL (129 mM)
Water ：55 mg/mL (182 mM)
Water ：55 mg/mL (182 mM)
外观
白色或类白色结晶性粉末
In vitro(体外研究)
Pramipexole, a chemically novel dopamine agonist used for the treatment of Parkinson's disease symptoms, possesses antioxidant activity and is neuroprotective toward substantia nigral dopamine neurons in hypoxic-ischemic and methamphetamine models. Pramipexole reduces the levels of oxygen radicals produced by methylpyridinium ion (MPP+) both when incubated with SH-SY5Y cells and when perfused into rat striatum. Pramipexole also exhibits a concentration-dependent inhibition of opening of the mitochondrial transition pore induced by calcium and phosphate or MPP+. Pramipexole decreases the levels of dopamine metabolites dose dependently, whereas striatal dopamine levels remains unchanged. Pramipexole acts in both of these models to reduce the elevated dopamine turnover and the associated elevation in hydroxyl radical production secondary to increased MAO activity that could be responsible for oxidative damage to the nigrostriatal neurons. Pramipexole (4-100 mM) significantly attenuates DA- or L-DOPA-induced cytotoxicity and apoptosis, an action which is not blocked by D3 antagonist U-99194 A or D2 antagonist raclopride. Pramipexole also protects MES 23.5 cells from hydrogen peroxide-induced cytotoxicity in a dose-dependent manner. Pramipexole can effectively inhibit the formation of melanin, an end product resulting from DA or L-DOPA oxidation in cell-free system.
In vivo(体内研究)
Pramipexole (0.001-1 mg/kg s.c.) reduces exploratory locomotor activity in mice. Pramipexole (1 mg/kg, p.o.) is able to significantly reduce the increased DA turnover, but by only 16%.
背景
别名
盐酸普拉克索
分子式
C10H17N3S.2HCl.H2O
CAS号
191217-81-9
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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